Medicinal Chemistry: A Key Driver in Achieving the Global Sustainable Development Goals

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: March 20, 2025

In 2015, the United Nations officially launched Sustainable Development Goals (SDGs) as "the blueprint to achieve a better and more sustainable future for all. They address global challenges we face, including those related poverty, inequality, climate change, environmental degradation, peace justice. The 17 are all interconnected, in order leave no one behind, it is important that them by 2030". Here, have embedded medicinal chemistry key player SDGs. We firmly believe can must contribute world with an improved quality of life taken critical look at each SDGs, dividing into Priority Foundational, analyzed how has impact on them. Although much been done, determined make progress this area.

Language: Английский

TogoPhosTAC: A Ready-To-Go and Adaptable Targeted Protein Dephosphorylation System

Research Square (Research Square), Journal Year: 2025, Volume and Issue: unknown

Published: March 25, 2025

Phosphorylation targeting chimeras (PhosTACs) recruit phosphatases to dephosphorylate target proteins by proximity-induced protein interactions. However, recruiting a phosphatase subunit or holoenzyme using small molecules without compromising its activity adversely disturbing cellular function remains challenging. In addition, many do not have favorable activator binder currently. To overcome these limitations, here, we report an adapted mode of action, named togoPhosTAC, based on the molecule PhosTAC, engineered fusion FKBP12^(F36V)-phosphatase, and lipid-based delivery system for targeted dephosphorylation. Through nanoparticles, delivered pre-fused complex PhosTACs FKBP12^(F36V)-phosphatases in mRNA format directly rapid efficient intracellular The togoPhosTAC was able epidermal growth factor receptor (EGFR), tau, α-synuclein. Furthermore, togoPhosTAC-mediated tau dephosphorylation also correlates with reduced aggregation. sum, our hybrid biologic adaptor strategy bypassed challenges ligand development provided alternative generalizable solution precise modulation in cellulo.

Language: Английский

PROTAC Technology as a New Tool for Modern Pharmacotherapy

Molecules, Journal Year: 2025, Volume and Issue: 30(10), P. 2123 - 2123

Published: May 11, 2025

The publication focuses on the innovative applications of PROTAC (proteolysis-targeting chimera) technology in modern pharmacotherapy, with particular emphasis cancer treatment. PROTACs represent an advanced therapeutic strategy that enables selective protein degradation, opening new possibilities drug design. This shows potential treatment cancers, viral infections (such as HIV and COVID-19), chronic diseases including atherosclerosis, Alzheimer’s disease, atopic dermatitis, Huntington’s disease. Promising results from clinical studies compound ARV-471 confirm effectiveness this approach. New types PROTACs, like TF-PROTAC PhosphoTAC, are designed to enhance effectiveness, stability, absorption drugs. conclusions review highlight broad various their relevance for future therapies, particularly oncology.

Language: Английский